Livedoksa - instructions for use, doses, side effects, contraindications

Excipients: lactose - 43,50 mg / 87,00 mg, starch - 9,00 mg / 18,00 mg, microcrystalline cellulose - 22,00 mg / 44,00 mg, sodium carboxymethyl starch - 13,00 mg / 26,00 mg, sodium lauryl sulfate - 3.00 mg / 6.00 mg, magnesium stearate - 3.00 mg / 6.00 mg, silicon dioxide colloid - 1.50 mg / 3.00 mg, talc purified - 6.40 mg / 12, 80 mg, povidone K-30 - 10.00 mg / 20.00 mg,

shell: (E5 premium) 4.80 mg / 9.60 mg, macrogol-6000 0.95 mg / 1.90 mg, titanium dioxide 0.48 mg / 0.96 mg, iron oxide yellow 0.08 mg / 0.16 mg, iron oxide red - 0.09 mg / 0.18 mg.

Description:

Round biconvex tablets brownish-red, film-coated, with a risk on one side.

View of the break: the core is white, surrounded by a brown-red shell.

Pharmacotherapeutic group:Hepatoprotective agent

ATX: & nbsp

A.05.A.A Preparations of bile acids

Pharmacodynamics:

Hepatoprotective agent also has choleretic, cholelitholytic, hypolipidemic, hypocholesterolemic and immunomodulating effects.Stabilizes membranes of hepatocytes and cholangiocytes, has a direct cytoprotective effect. As a result of the drug on the gastrointestinal circulation of bile acids, the content of hydrophobic (potentially toxic) acids decreases. By reducing the absorption of cholesterol in the intestine and other biochemical effects has a hypocholesterolemic effect. Suppresses cell death due to toxic bile acids.

Possessing high polar properties, ursodeoxycholic acid (UDCA) forms non-toxic mixed micelles with apolar (toxic) bile acids, which reduces the ability of gastric reflux to damage cell membranes with biliary reflux gastritis and reflux esophagitis. In addition, UDCA forms double molecules that can be included in the composition of cell membranes, stabilize them and make them immune to the action of cytotoxic micelles. Reduces the saturation of bile with cholesterol due to inhibition of its absorption in the intestine, suppression of synthesis in the liver and a decrease in secretion in bile; increases the solubility of cholesterol in bile, forming with it liquid crystals; reduces the lithogenic bile index.The result is the dissolution of cholesterol gallstones (the effect of changing the cholesterol / bile acid ratio in bile) and the prevention of the formation of new stones (the result of a decrease in the content in bile cholesterol). It induces choleresis, rich in bicarbonates, which leads to an increase in bile passage and stimulates the excretion of toxic bile acids through the intestine.

Immunomodulatory effect due to oppression of expression HLAantigens (HLA - human leucocyte antigens - tissue compatibility antigens) on the membranes of hepatocytes and cholangiocytes, normalization of the natural killer activity of lymphocytes, etc. Reliably delay the progression of fibrosis in patients with primary biliary cirrhosis, cystic fibrosis and alcoholic steatohepatitis, reduces the risk of developing varicose veins of the esophagus.

Pharmacokinetics:

Absorption and distribution.

UDCA is absorbed from the jejunum due to passive diffusion, and from the ileum through active transport. Penetrates through the placental barrier. Concentration in the plasma with oral administration of 500 mg is achieved after 30, 60, 90 minutes - 3.8, 5.5, 3.7 mmol / l, respectively.The distribution of UDCA characterizes a high degree of binding to plasma proteins, which can be 96- 99%.

Metabolism and excretion.

As a result of presystemic elimination of UDCA, taurine and glycine conjugates are formed, which are secreted in bile. About 50 to 70% of the entire administered dose of UDCA is excreted with bile. The remainder of the non-absorbed fraction of UDCA enters the large intestine, where it undergoes bacterial cleavage (7-dehydroxylation) to form lithocholic acid. Litocholic acid is partially absorbed from the intestine, biotransformed in the liver into sulfolithocholylglycine and sulfolitocholyltaurine conjugates and is excreted.

Indications:

- Primary biliary cirrhosis in the absence of signs of decompensation (symptomatic therapy);

- Dissolution of small and medium cholesterol stones with a functioning gallbladder;

- Biliary reflux-gastritis and reflux esophagitis;

- Chronic hepatitis of various genesis;

- Alcoholic liver disease;

- Non-alcoholic steatohepatitis;

- Primary sclerosing cholangitis;

- Cystic fibrosis (cystic fibrosis);

- Dyskinesia of bile ducts.

Contraindications:

- Increased individual sensitivity to the components of the drug;

- X-ray positive (high in calcium) gallstones;

- non-functioning gallbladder;

- acute inflammatory diseases of the gallbladder, bile ducts and intestines;

- cirrhosis of the liver in the stage of decompensation;

- marked violations of the kidneys, liver, pancreas;

lactose intolerance;

- deficiency of lactase or glucose-galactose malabsorption;

- Children under 3 years old.

Carefully:

Carefully used in children aged 3 to 4 years, t. may be difficult if the tablets are swallowed, although ursodeoxycholic acid has no age restrictions in the application.

Pregnancy and lactation:

The use of ursodeoxycholic acid in pregnancy is possible only if the expected benefit for the mother exceeds the potential risk for the fetus (adequate strictly controlled studies of the use of ursodeoxycholic acid in pregnant women have not been conducted).

Data on the isolation of ursodeoxycholic acid with breast milk are currently not available.If it is necessary to use ursodeoxycholic acid during lactation, the question of stopping breastfeeding should be solved.

Dosing and Administration:

Lividoks ® tablets are taken orally, without chewing, with enough water. A tablet can be divided in half.

To dissolve cholesteric gallstones the average daily dose of Livedaxa ® is 10 mg / kg (up to 12-15 mg / kg). The drug is taken in the evening, before going to bed. The course of treatment is 6-12 months. For the prevention of repeated formation of stones, it is recommended to take the drug for several months after the dissolution of the stones.

Symptomatic therapy of primary biliary cirrhosis: the average daily dose is 10-15 mg / kg (if necessary - up to 20 mg / kg) from 6 months to several years. The drug is taken with food, squeezed with enough liquid.

With biliary reflux gastritis and reflux esophagitis the dose is 10 mg / kg / day - 1 time a day before bedtime. The course of treatment - from 10-14 days to 6 months, if necessary - up to 2 years.

With chronic hepatitis of various origins (toxic, medicinal, etc.), primary nonalcoholic steatohepatitis, alcoholic liver disease the average daily dose is 10-15 mg / kg body weight in 2-3 doses. The duration of therapy is 6-12 months or more.

With primary sclerosing cholangitis, cystic fibrosis (cystic fibrosis) the average daily dose is 12-15 mg / kg (for of necessity - up to 20-30 mg / kg / day) in 2-3 doses. The duration of therapy is from 6 months to several years.

With dyskinesia biliary tract the average daily dose is 10 mg / kg in 2 divided doses for 2 weeks to 2 months. If necessary, the course of treatment is recommended to be repeated.

Children older than 3 years ursodeoxycholic acid is administered individually, at a rate of 10-20 mg / kg / day.

Calculating the daily amount of tablets Livedovax® 150 mg, depending on the patient's body weight and the recommended dose of the drug per 1 kg of body weight:

Body weight, kg	10 mg / kg / day	15 mg / kg / day
34-50	3 tab.	5 tab.
51-65	4 tab.	6 tab.
66-85	5 tab.	7 tab.
86-100	6 tab.	9 tab.

Calculating the daily amount of tablets LIVELX ® 300 mg, depending on the patient's body weight and the recommended dose of the drug per 1 kg of body weight:

Weight body, kg	10 mg / kg / day	15 mg / kg / day	20 mg / kg / day	30 mg / kg / day
34-50	1.5 tab.	2 tab.	3 tab.	5 tab.
51-65	2 tab.	3 tab.	4 tab.	6 tab.
66-85	2.5 tab.	3.5 tab.	5 tab.	7 tab.
86-100	3 tab.	4,5 tab.	6 tab.	8 tab.
>100	4 tab.	6 tab.	7 tab.	9 tab.

Side effects:

Calcification of gallstones, increased activity of "liver" transaminases, allergic reactions (including urticaria), diarrhea, nausea, abdominal pain; in the treatment of primary biliary cirrhosis, transient decompensation of liver cirrhosis that occurs after the drug cancellation can be observed.

Overdose:Cases of overdose UDCA are not known.

Interaction:

Do not use the drug simultaneously with antacids containing aluminum and ion exchange resins, because these drugs can disrupt the absorption of ursodeoxycholic acid. With the simultaneous use of lipid-lowering drugs agents, estrogens, neomycin or progestogens (oral contraceptives) increase the saturation of bile cholesterol and can reduce the ability of ursodeoxycholic acid to dissolve cholesterol biliary calculi.

Ursodeoxycholic acid can increase the absorption of cyclosporine from the intestine, which requires monitoring the concentration of cyclosporine in the blood, and, if necessary, correcting its dosage regimen.

Special instructions:

To successfully dissolve it is necessary that the stones are pure cholesterol, not more than 15-20 mm in size, the gallbladder is filled with stones no more than half and the bile ducts fully retained their function. At the appointment with the purpose of dissolution of gallstones, it is necessary to control the activity of "liver" transaminases and alkaline phosphatase, gamma-glutamyl transpeptidase, bilirubin concentrations. If the increased indices remain, the drug should be discontinued.

Cholecystography should be performed every 4 weeks in the first 3 months of treatment, then every 3 months. Control of treatment effectiveness should be performed every 6 months during ultrasound during the first year of therapy. After complete dissolution of the stones, it is recommended to continue the application at for at least 3 months, in order to promote dissolution. Remains of stones, the size of which is too small for their detection.

If within 6-12 months after the beginning of therapy of partial dissolution of concrements did not occur, it is unlikely that the treatment will be effective.

Detection during treatment of a nonvisualizable gallbladder is evidence that no complete dissolution of the calculi has occurred, and treatment should be discontinued.

When calcification of gallstones, violation of the contractility of the gallbladder or frequent attacks of biliary colic, treatment should be discontinued.

Effect on the ability to drive transp. cf. and fur:

There is no data on the impact of UDCA on the ability to drive vehicles and work with machinery.

Form release / dosage:Tablets, film-coated 150 mg and 300 mg.

Packaging:

10 tablets per blister, made of PVC and aluminum foil.

For 1, 5, 6, 9, 10 or 12 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008974/10

Date of registration:31.08.2010 / 22.01.2015

Expiration Date:Unlimited

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp28.02.2018

Illustrated instructions

Instructions

LIVELAX® (Livodexa)